The biotransformation of [14C]minaprine in man and five animals species.
1. [14C]Minaprine was administered as a single oral dose to five animal species and to a healthy and informed volunteer. Excretion of radioactivity was followed during 48 h in urine and faces; biliary excretion was followed only in rat. 2. Urinary metabolites were isolated and identified by mass spectrometry. 3. A quantitative comparison of metabolites in different species was made. On the basis of these data it it concluded that the dog is not a suitable model for man for pharmacological or toxicological studies. 4. The major metabolic route is 4-hydroxylation of the aromatic ring. The only unexpected metabolic route found was the biotransformation of the morpholino ring, probably by reductive ring-cleavage. 5. About 50% of the 14C was excreted in 0-48 h urine. The other 50% was excreted in the 0-48 h faces. In the rat, this was attribute entirely to biliary excretion. The drug is well absorbed after oral administration and is not accumulated in the body.
D000328:Adult; D000818:Animals; D000928:Antidepressive Agents / Q000378:metabolism*; D001711:Biotransformation; D002143:Callitrichinae; D002855:Chromatography, Thin Layer; D004285:Dogs; D005260:Female; D008401:Gas Chromatography-Mass Spectrometry; D006801:Humans; D008252:Macaca fascicularis; D008297:Male; D009025:Morpholines / Q000378:metabolism; D010215:Papio; D011724:Pyridazines / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D013045:Species Specificity
D000928:Antidepressive Agents; D009025:Morpholines; D011724:Pyridazines; C006149:minaprine